WO2011115940A1 - Substituted pyrimidines as prostaglandin d2 receptor antagonists - Google Patents

Substituted pyrimidines as prostaglandin d2 receptor antagonists Download PDF

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Publication number
WO2011115940A1
WO2011115940A1 PCT/US2011/028427 US2011028427W WO2011115940A1 WO 2011115940 A1 WO2011115940 A1 WO 2011115940A1 US 2011028427 W US2011028427 W US 2011028427W WO 2011115940 A1 WO2011115940 A1 WO 2011115940A1
Authority
WO
WIPO (PCT)
Prior art keywords
phenyl
methoxy
trifluoromethoxy
pyrimidin
ethylamino
Prior art date
Application number
PCT/US2011/028427
Other languages
English (en)
French (fr)
Inventor
Keith J. Harris
Joacy C. Aguiar
Patrick Wai-Kwok Shum
Zhicheng Zhao
Gregory B. Poli
Gregory Stoklosa
Yong-Mi Choi-Sledeski
Stephan Reiling
David Stefany
Charles Gardner
Original Assignee
Aventis Pharmaceuticals Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to EP11710373A priority Critical patent/EP2547672A1/en
Priority to CN2011800243826A priority patent/CN103038228A/zh
Priority to SG2012063913A priority patent/SG183533A1/en
Priority to AU2011227417A priority patent/AU2011227417A1/en
Priority to RU2012143897/04A priority patent/RU2012143897A/ru
Priority to KR1020127026848A priority patent/KR20130018770A/ko
Application filed by Aventis Pharmaceuticals Inc. filed Critical Aventis Pharmaceuticals Inc.
Priority to MX2012010035A priority patent/MX2012010035A/es
Priority to BR112012023178A priority patent/BR112012023178A2/pt
Priority to CA2793223A priority patent/CA2793223A1/en
Priority to JP2013500142A priority patent/JP2013522306A/ja
Publication of WO2011115940A1 publication Critical patent/WO2011115940A1/en
Priority to US13/610,027 priority patent/US20130005728A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
PCT/US2011/028427 2010-03-16 2011-03-15 Substituted pyrimidines as prostaglandin d2 receptor antagonists WO2011115940A1 (en)

Priority Applications (11)

Application Number Priority Date Filing Date Title
CN2011800243826A CN103038228A (zh) 2010-03-16 2011-03-15 作为前列腺素d2受体拮抗剂的取代的嘧啶类化合物
SG2012063913A SG183533A1 (en) 2010-03-16 2011-03-15 Substituted pyrimidines as prostaglandin d2 receptor antagonists
AU2011227417A AU2011227417A1 (en) 2010-03-16 2011-03-15 Substituted pyrimidines as prostaglandin D2 receptor antagonists
RU2012143897/04A RU2012143897A (ru) 2010-03-16 2011-03-15 Замещенные пиримидины как антагонисты рецепторов простагландина d2
KR1020127026848A KR20130018770A (ko) 2010-03-16 2011-03-15 프로스타글란딘 ｄ２ 수용체 길항제들로서의 치환된 피리미딘들
EP11710373A EP2547672A1 (en) 2010-03-16 2011-03-15 Substituted pyrimidines as prostaglandin d2 receptor antagonists
MX2012010035A MX2012010035A (es) 2010-03-16 2011-03-15 Pirimidinas sustituidas como antagonistas del receptor de la prostaglandina d2.
BR112012023178A BR112012023178A2 (pt) 2010-03-16 2011-03-15 ramidinas substituídas como antagonistas de receptor prostaglandina 2
CA2793223A CA2793223A1 (en) 2010-03-16 2011-03-15 Substituted pyrimidines as prostaglandin d2 receptor antagonists
JP2013500142A JP2013522306A (ja) 2010-03-16 2011-03-15 プロスタグランジンｄ２受容体アンタゴニストとしての置換ピリミジン類
US13/610,027 US20130005728A1 (en) 2010-03-16 2012-09-11 Substituted pyrimidines as prostaglandin d2 receptor antagonists

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31442810P 2010-03-16 2010-03-16
US61/314,428 2010-03-16

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US13/610,027 Continuation US20130005728A1 (en) 2010-03-16 2012-09-11 Substituted pyrimidines as prostaglandin d2 receptor antagonists

Publications (1)

Publication Number Publication Date
WO2011115940A1 true WO2011115940A1 (en) 2011-09-22

Family

ID=43983955

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/028427 WO2011115940A1 (en) 2010-03-16 2011-03-15 Substituted pyrimidines as prostaglandin d2 receptor antagonists

Country Status (15)

Country Link
US (1) US20130005728A1 (ja)
EP (1) EP2547672A1 (ja)
JP (1) JP2013522306A (ja)
KR (1) KR20130018770A (ja)
CN (1) CN103038228A (ja)
AR (1) AR080590A1 (ja)
AU (1) AU2011227417A1 (ja)
BR (1) BR112012023178A2 (ja)
CA (1) CA2793223A1 (ja)
MX (1) MX2012010035A (ja)
RU (1) RU2012143897A (ja)
SG (1) SG183533A1 (ja)
TW (1) TW201200133A (ja)
UY (1) UY33278A (ja)
WO (1) WO2011115940A1 (ja)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2563359A1 (en) * 2010-04-30 2013-03-06 Allergan, Inc. Novel treatment for age related macular degeneration and ocular ischemic disease associated with complement activation by targeting 5-lipoxygenase
US10683293B2 (en) 2014-08-04 2020-06-16 Nuevolution A/S Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
US11447479B2 (en) 2019-12-20 2022-09-20 Nuevolution A/S Compounds active towards nuclear receptors
US11613532B2 (en) 2020-03-31 2023-03-28 Nuevolution A/S Compounds active towards nuclear receptors
US11780843B2 (en) 2020-03-31 2023-10-10 Nuevolution A/S Compounds active towards nuclear receptors
US11926616B2 (en) 2018-03-08 2024-03-12 Incyte Corporation Aminopyrazine diol compounds as PI3K-γ inhibitors

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US9797903B2 (en) 2012-10-24 2017-10-24 Winthrop-University Hospital Non-invasive biomarker to identify subject at risk of preterm delivery
CN105439964B (zh) * 2015-12-09 2019-02-15 河北大学 一种阿伐那非中间体的制备方法
DE102016216163B4 (de) * 2016-08-29 2019-11-14 Siemens Healthcare Gmbh Verfahren zur Korrektur einer Signalphase bei der Aufnahme von Magnetresonanzsignalen, Magnetresonanzeinrichtung, Computerprogramm und Datenträger
AU2018331400A1 (en) 2017-09-13 2020-04-02 Progenity, Inc. Preeclampsia biomarkers and related systems and methods
EP4070113A4 (en) 2019-12-04 2023-12-20 Biora Therapeutics, Inc. ASSESSMENT OF PREECAMPSIA USING FREE AND DISSOCIATE PLACENTAL GROWTH FACTOR ASSAYS

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WO2007121280A1 (en) * 2006-04-12 2007-10-25 Sanofi-Aventis 2,6-substituted-4-monosubstituted amino-pyrimidine as prostaglandin d2 receptor antagonists
WO2008039882A1 (en) * 2006-09-30 2008-04-03 Sanofi-Aventis U.S. Llc A combination of niacin and a prostaglandin d2 receptor antagonist

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Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2563359A1 (en) * 2010-04-30 2013-03-06 Allergan, Inc. Novel treatment for age related macular degeneration and ocular ischemic disease associated with complement activation by targeting 5-lipoxygenase
US10683293B2 (en) 2014-08-04 2020-06-16 Nuevolution A/S Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases
US10689383B2 (en) 2014-08-04 2020-06-23 Nuevolution A/S Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases
US11254681B2 (en) 2014-08-04 2022-02-22 Nuevolution A/S Optionally fused heterocyclyl-substituted derivatives of pyrimidine useful for the treatment of inflammatory, metabolic, oncologic and autoimmune diseases
US11926616B2 (en) 2018-03-08 2024-03-12 Incyte Corporation Aminopyrazine diol compounds as PI3K-γ inhibitors
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
US11447479B2 (en) 2019-12-20 2022-09-20 Nuevolution A/S Compounds active towards nuclear receptors
US11613532B2 (en) 2020-03-31 2023-03-28 Nuevolution A/S Compounds active towards nuclear receptors
US11780843B2 (en) 2020-03-31 2023-10-10 Nuevolution A/S Compounds active towards nuclear receptors

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BR112012023178A2 (pt) 2019-09-24
AR080590A1 (es) 2012-04-18
JP2013522306A (ja) 2013-06-13
CN103038228A (zh) 2013-04-10
SG183533A1 (en) 2012-10-30
TW201200133A (en) 2012-01-01
KR20130018770A (ko) 2013-02-25
MX2012010035A (es) 2012-10-01
RU2012143897A (ru) 2014-04-27
EP2547672A1 (en) 2013-01-23
CA2793223A1 (en) 2011-09-22
AU2011227417A1 (en) 2012-10-11
UY33278A (es) 2011-10-31
US20130005728A1 (en) 2013-01-03

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